title: Mono-carbonyl curcumin analogues as 11β-hydroxysteroid dehydrogenase 1 inhibitors.
abstract: A series of structurally novel mono-carbonyl curcumin analogues have been synthesized and biologically evaluated to test their inhibitory potencies and the structure-activity relationship (SAR) on human and rat 11β-hydroxysteroid dehydrogenase isoform (11β-HSD1) activities. 11β-HSD1 selective inhibitors have been discovered and compound A10 is discovered as a very potent with an IC50 value of 97 nM without inhibiting 11β-HSD2.
authors.affiliation: The 2nd Affiliated Hospital & Institute of Reproductive Biomedicine, Wenzhou Medical College, Wenzhou 325000, China.
authors.forename: Han
authors.initials: H
authors.lastname: Lin
authors.forename: Guo-Xin
authors.initials: GX
authors.lastname: Hu
authors.forename: Jingjing
authors.initials: J
authors.lastname: Guo
authors.forename: Yufei
authors.initials: Y
authors.lastname: Ge
authors.forename: Guang
authors.initials: G
authors.lastname: Liang
authors.forename: Qing-Quan
authors.initials: QQ
authors.lastname: Lian
authors.forename: Yanhui
authors.initials: Y
authors.lastname: Chu
authors.forename: Xiaohuan
authors.initials: X
authors.lastname: Yuan
authors.forename: Ping
authors.initials: P
authors.lastname: Huang
authors.forename: Ren-Shan
authors.initials: RS
authors.lastname: Ge
mesh_terms: D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D043209:11-beta-Hydroxysteroid Dehydrogenase Type 2 / Q000037:antagonists & inhibitors / Q000378:metabolism; D000818:Animals; D003474:Curcumin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism; D006801:Humans; D008861:Microsomes / Q000378:metabolism; D011485:Protein Binding; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1; D043209:11-beta-Hydroxysteroid Dehydrogenase Type 2; D003474:Curcumin